KR20120083416A - 아자비시클릭 화합물의 제조 방법 - Google Patents

아자비시클릭 화합물의 제조 방법 Download PDF

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Publication number
KR20120083416A
KR20120083416A KR1020127009689A KR20127009689A KR20120083416A KR 20120083416 A KR20120083416 A KR 20120083416A KR 1020127009689 A KR1020127009689 A KR 1020127009689A KR 20127009689 A KR20127009689 A KR 20127009689A KR 20120083416 A KR20120083416 A KR 20120083416A
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KR
South Korea
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compound
formula
solvent
mixture
base
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KR1020127009689A
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English (en)
Korean (ko)
Inventor
나렌드라 발칸드라 암바이카르
브리안 리차드 베어
레브 티. 디. 패닝
로버트 휴즈
벤자민 리틀러
Original Assignee
버텍스 파마슈티칼스 인코포레이티드
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Publication of KR20120083416A publication Critical patent/KR20120083416A/ko
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B61/00—Other general methods
    • C07B61/02—Generation of organic free radicals; Organic free radicals per se
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/33—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C211/34—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton
    • C07C211/35—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing only non-condensed rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020127009689A 2009-09-17 2010-09-17 아자비시클릭 화합물의 제조 방법 Withdrawn KR20120083416A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24347709P 2009-09-17 2009-09-17
US61/243,477 2009-09-17

Publications (1)

Publication Number Publication Date
KR20120083416A true KR20120083416A (ko) 2012-07-25

Family

ID=43242763

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020127009689A Withdrawn KR20120083416A (ko) 2009-09-17 2010-09-17 아자비시클릭 화합물의 제조 방법

Country Status (15)

Country Link
US (2) US8404865B2 (enrdf_load_stackoverflow)
EP (1) EP2477991B1 (enrdf_load_stackoverflow)
JP (1) JP5793496B2 (enrdf_load_stackoverflow)
KR (1) KR20120083416A (enrdf_load_stackoverflow)
CN (1) CN102498112B (enrdf_load_stackoverflow)
AU (1) AU2010295461B2 (enrdf_load_stackoverflow)
BR (1) BR112012006031A2 (enrdf_load_stackoverflow)
CA (1) CA2772792A1 (enrdf_load_stackoverflow)
ES (1) ES2540810T3 (enrdf_load_stackoverflow)
IL (1) IL218641A0 (enrdf_load_stackoverflow)
MX (1) MX2012003343A (enrdf_load_stackoverflow)
NZ (1) NZ598277A (enrdf_load_stackoverflow)
RU (1) RU2543622C2 (enrdf_load_stackoverflow)
WO (1) WO2011035139A1 (enrdf_load_stackoverflow)
ZA (1) ZA201201252B (enrdf_load_stackoverflow)

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WO2005049018A1 (en) * 2003-11-14 2005-06-02 Vertex Pharmaceuticals Incorporated Thiazoles and oxazoles useful as modulators of atp-binding cassette transporters
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
WO2007056341A1 (en) * 2005-11-08 2007-05-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
ME02970B (me) 2004-06-24 2018-07-20 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
NZ566208A (en) 2005-08-11 2010-09-30 Vertex Pharma 2-Thiazolamide derivatives as modulators of cystic fibrosis transmembrane conductance regulators
CA2635581C (en) 2005-12-28 2017-02-28 Vertex Pharmaceuticals Incorporated Solid forms of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
CA2856037C (en) * 2005-12-28 2017-03-07 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
WO2007117715A2 (en) 2006-04-07 2007-10-18 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
US8969386B2 (en) 2007-05-09 2015-03-03 Vertex Pharmaceuticals Incorporated Modulators of CFTR
HUE028426T2 (en) 2007-08-24 2016-12-28 Vertex Pharma Isothiazolopyridinones for (inter alia) treating cystic fibrosis
NZ598941A (en) 2007-11-16 2013-06-28 Vertex Pharma Isoquinoline modulators of ATP-Binding Cassette transporters
WO2009076142A2 (en) * 2007-12-07 2009-06-18 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxiamido-pyridine benzoic acids
UA102534C2 (xx) 2007-12-07 2013-07-25 Вертекс Фармасьютикалз Инкорпорейтед ТВЕРДА ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДІОКСОЛ-5-ІЛ)-ЦИКЛОПРОПАНКАРБОКСАМІДО)-3-МЕТИЛПІРИДИН-2-ІЛ)БЕНЗОЙНОЇ КИСЛОТИ (ВАРІАНТИ)$ТВЕРДАЯ ФОРМА 3-(6-(1-(2,2-ДИФТОРБЕНЗО$d]$1,3]-ДИОКСОЛ-5-ИЛ)-ЦИКЛОПРОПАНКАРБОКСАМИДО)-3-МЕТИЛПИРИДИН-2-ИЛ)БЕНЗОЙНОЙ КИСЛОТЫ (ВАРИАНТЫ)
AU2008335439A1 (en) * 2007-12-07 2009-06-18 Vertex Pharmaceuticals Incorporated Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
WO2009108657A2 (en) * 2008-02-28 2009-09-03 Vertex Pharmaceuticals Incorporated Heteroaryl derivatives as cftr modulators
CA2718310C (en) 2008-03-31 2018-08-07 Vertex Pharmaceuticals Incorporated Pyridyl derivatives as cftr modulators
BRPI0919550A2 (pt) * 2008-09-29 2019-09-10 Vertex Pharma unidades de dosagem de ácido 3-(6-(1-(2,2-difluorobenzo]d][1,3]dioxol-5-il)ciclopropanocarboxamido)-3-metilpiridin-2-il)benzoico
UA104601C2 (uk) 2008-10-23 2014-02-25 Вертекс Фармасьютікалз, Інкорпорейтед Модулятори регулятора трансмембранної провідності при муковісцидозі
MX361711B (es) 2009-03-20 2018-12-14 Vertex Pharmaceuticals Incorporated Star Proceso para producir moduladores del regulador de conductancia transmembrana de fibrosis quistica.
ES2540810T3 (es) * 2009-09-17 2015-07-13 Vertex Pharmaceuticals Incorporated Proceso para preparar compuestos azabicíclicos
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
TWI549950B (zh) 2010-04-07 2016-09-21 維泰克斯製藥公司 ３－（６－（１－（２，２－二氟苯并［ｄ］［１，３］二氧雜環戊烯－５－基）環丙烷甲醯胺基）－３－甲基吡啶－２－基）苯甲酸之固體形式
US8552034B2 (en) 2010-04-07 2013-10-08 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid and administration thereof
ES2608474T3 (es) 2010-04-22 2017-04-11 Vertex Pharmaceuticals Incorporated Proceso de producción de compuestos indol cycloalkylcarboxamido
CA2796642A1 (en) 2010-04-22 2011-10-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions and administrations thereof
NZ603043A (en) 2010-04-22 2015-02-27 Vertex Pharma Pharmaceutical compositions comprising cftr modulators and administrations thereof
US8563593B2 (en) 2010-06-08 2013-10-22 Vertex Pharmaceuticals Incorporated Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide
US9254291B2 (en) 2011-11-08 2016-02-09 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
IL311180A (en) 2012-02-27 2024-04-01 Vertex Pharma Pharmaceutical preparations containing a solid dispersion of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide and uses thereof
CN102633804B (zh) * 2012-04-19 2014-09-24 中南大学 一种制备7-氮杂双环[2.2.1]庚烷的方法
US8674108B2 (en) 2012-04-20 2014-03-18 Vertex Pharmaceuticals Incorporated Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
HK1209318A1 (en) 2012-07-16 2016-04-01 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of (r)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration thereof
RU2718044C2 (ru) 2013-11-12 2020-03-30 Вертекс Фармасьютикалз Инкорпорейтед Способ получения фармацевтических композиций для лечения опосредованных cftr заболеваний
MX387720B (es) 2014-04-15 2025-03-12 Vertex Pharma Composiciones farmacéuticas para el tratamiento de enfermedades mediadas por el regulador de conductancia de transmembrana de fibrosis quística.
US9701639B2 (en) 2014-10-07 2017-07-11 Vertex Pharmaceuticals Incorporated Co-crystals of modulators of cystic fibrosis transmembrane conductance regulator
KR102576006B1 (ko) 2014-11-18 2023-09-06 버텍스 파마슈티칼스 인코포레이티드 고처리량 시험 고성능 액체 크로마토그래피의 수행 방법
CR20230120A (es) 2020-08-07 2023-09-01 Vertex Pharma Moduladores del regulador de la conductancia transmembrana de la fibrosis quística
US12324802B2 (en) 2020-11-18 2025-06-10 Vertex Pharmaceuticals Incorporated Modulators of cystic fibrosis transmembrane conductance regulator

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JPH06312989A (ja) * 1993-04-30 1994-11-08 Nippon Chemiphar Co Ltd （１ｒｓ，２ｒｓ，４ｓｒ）−２−（６−クロロ−３−ピリジル）−７−アザビシクロ［２．２．１］ヘプタンの製造方法
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ME02970B (me) 2004-06-24 2018-07-20 Vertex Pharma Modulatori atp-vezujućih kasetnih transportera
EP1844040A1 (en) * 2005-01-21 2007-10-17 Pfizer Limited Crystalline forms of cis-5-fluoro-n-[4-(2-hydroxy-4-methylbenzamido)cyclohexyl]-2-(tetrahydrothiopyran-4-yloxy)nicotinamide
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UA104601C2 (uk) 2008-10-23 2014-02-25 Вертекс Фармасьютікалз, Інкорпорейтед Модулятори регулятора трансмембранної провідності при муковісцидозі
ES2540810T3 (es) * 2009-09-17 2015-07-13 Vertex Pharmaceuticals Incorporated Proceso para preparar compuestos azabicíclicos
NZ599703A (en) * 2009-10-23 2014-06-27 Vertex Pharma Solid forms of n-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide
WO2011050215A1 (en) * 2009-10-23 2011-04-28 Vertex Pharmaceuticals Incorporated Process for preparing modulators of cystic fibrosis transmembrane conductance regulator
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Also Published As

Publication number Publication date
US20110065928A1 (en) 2011-03-17
ZA201201252B (en) 2013-05-29
IL218641A0 (en) 2012-05-31
BR112012006031A2 (pt) 2019-09-24
RU2012115111A (ru) 2013-10-27
AU2010295461A1 (en) 2012-03-08
NZ598277A (en) 2014-03-28
EP2477991B1 (en) 2015-04-15
JP2013505259A (ja) 2013-02-14
ES2540810T3 (es) 2015-07-13
EP2477991A1 (en) 2012-07-25
US20120259129A1 (en) 2012-10-11
CN102498112B (zh) 2015-05-20
RU2543622C2 (ru) 2015-03-10
AU2010295461B2 (en) 2016-03-03
US8404865B2 (en) 2013-03-26
MX2012003343A (es) 2012-08-17
JP5793496B2 (ja) 2015-10-14
CA2772792A1 (en) 2011-03-24
US8461352B2 (en) 2013-06-11
HK1169106A1 (en) 2013-01-18
CN102498112A (zh) 2012-06-13
WO2011035139A1 (en) 2011-03-24

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Patent event date: 20120416

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